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3-[(E)-(acridin-9′-ylmethylidene)amino]-1-substituted thioureas and their biological activity.

Autor: Bečka M., Vilková M., Salem O., Kašpárková J., Brabec V., Kožurková M.Published: Spectrochimica Acta Part A: Molecular and Biomolecular Spectroscopy 180, 234-241Year: 2017

This paper describes the synthesis of a novel series of acridine thiosemicarbazones through a two-step reaction between various isothiocyanates and hydrazine followed by treatment with acridin-9-carbaldehyde. The properties of this series of seven new derivatives are studied using NMR and biochemical techniques, and the DNA-binding properties of the compounds are determined using spectrophotometric studies (UV–vis absorption, fluorescence, and circular/linear dichroism) and viscometry. The binding constants K are estimated as being in the range of 2.2 to 7.8 × 104 M−1 and the percentage of hypochromism was found to be 22.11–49.75% (from UV–vis spectral titration). Electrophoretic experiments prove that the novel compounds demonstrate moderate inhibitory effects against Topo I activity at a concentration of 60 × 10−6 M.

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